US11433090B2ActiveUtilityA1

mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof

82
Assignee: THE DOSHISHAPriority: Jun 16, 2017Filed: Jun 15, 2018Granted: Sep 6, 2022
Est. expiryJun 16, 2037(~10.9 yrs left)· nominal 20-yr term from priority
A61K 31/7088A61K 31/436A61P 27/02A61K 31/7105A61K 31/711A61K 31/713A61K 45/06A61P 43/00A61K 45/00A61K 9/0048
82
PatentIndex Score
1
Cited by
216
References
16
Claims

Abstract

The present invention provides a medicine and a method for preventing or treating ophthalmic symptoms, disorders, or diseases. The present invention provides an mTOR-inhibitor-containing composition for preventing or treating ophthalmic symptoms, disorders, or diseases. In some of the embodiments of the present invention, this composition is capable of treating or preventing corneal endothelial symptoms, disorders, or diseases; in particular, corneal endothelial symptoms, disorders, or diseases that are attributed to overexpression of the transforming growth factor-β (TGF-β) signal and/or extracellular matrix (ECM).

Claims

exact text as granted — not AI-modified
The invention claimed is: 
     
       1. A method for preventing or treating an eye condition, disorder, or disease in a subject, wherein the method comprises administering an effective amount of an mTOR inhibitor to the subject, wherein the eye condition, disorder, or disease is a corneal endothelial condition, disorder, or disease due to a transforming growth factor-β (TGF-β). 
     
     
       2. The method of  claim 1 , wherein the corneal endothelial condition, disorder, or disease is selected from the group consisting of Fuchs' endothelial corneal dystrophy, post-corneal transplant disorder, corneal endotheliitis, trauma, ophthalmic surgery, post-ophthalmic laser surgery disorder, aging, posterior polymorphous dystrophy (PPD), congenital hereditary endothelial dystrophy (CHED), idiopathic corneal endothelial disorder, and cytomegalovirus corneal endotheliitis. 
     
     
       3. The method of  claim 1 , wherein the corneal endothelial condition, disorder, or disease is due to overexpression of extracellular matrix (ECM). 
     
     
       4. The method of  claim 3 , wherein the corneal endothelial condition, disorder, or disease is selected from the group consisting of Fuchs' endothelial corneal dystrophy, guttae formation, hypertrophy of a Descemet's membrane, hypertrophy of a cornea, turbidity, scar, corneal nebula, corneal macula, leucoma, photophobia, and blurred vision. 
     
     
       5. The method of  claim 1 , wherein the condition, disorder, or disease comprises Fuchs' endothelial corneal dystrophy. 
     
     
       6. The method of  claim 1 , wherein the mTOR inhibitor is selected from the group consisting of rapamycin, temsirolimus, everolimus, PI-103, CC-223, INK128, AZD8055, KU 0063794, Voxtalisib, Ridaforolimus, NVP-BEZ235, CZ415, Torkinib, Torin 1, Omipalisib, OSI-027, PF-04691502, Apitolisib, WYE-354, Vistusertib, Torin 2, Tacrolimus, GSK1059615, Gedatolisib, WYE-125132, BGT226, Palomid 529, PP121, WYE-687, CH5132799, WAY-600, ETP-46464, GDC-0349, XL388, Zotarolimus, and Chrysophanic Acid. 
     
     
       7. The method of  claim 1 , wherein the mTOR inhibitor is selected from the group consisting of rapamycin, temsirolimus, and everolimus. 
     
     
       8. The method of  claim 1 , wherein the mTOR inhibitor is administered as an eye drop. 
     
     
       9. The method of  claim 1 , wherein the mTOR inhibitor is rapamycin and is administered as an eye drop at least about 0.1 nM. 
     
     
       10. The method of  claim 1 , wherein the mTOR inhibitor is administered as an eye drop, wherein the mTOR inhibitor is rapamycin and is present in the eye drop at least about 0.1 mM. 
     
     
       11. The method of  claim 1 , wherein the mTOR inhibitor is temsirolimus and is administered as an eye drop at least about 0.01 nM. 
     
     
       12. The method of  claim 1 , wherein the mTOR inhibitor is administered as an eye drop, wherein the mTOR inhibitor is temsirolimus and is present in the eye drop at least about 0.01 mM. 
     
     
       13. The method of  claim 1 , wherein the mTOR inhibitor is everolimus and is administered as an eye drop at least about 0.1 nM. 
     
     
       14. The method of  claim 1 , wherein the mTOR inhibitor is administered as an eye drop, wherein the mTOR inhibitor is everolimus and is present in the eye drop at least about 0.1 mM. 
     
     
       15. A method for preventing or treating an eye condition, disorder, or disease in a subject, wherein the method consists essentially of administering an effective amount of an mTOR inhibitor to the subject, wherein the eye condition, disorder, or disease is a corneal endothelial condition, disorder, or disease due to a transforming growth factor-β (TGF-β). 
     
     
       16. The method of  claim 15 , wherein the mTOR inhibitor is rapamycin.

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